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Carbonic anhydrase inhibitors.
The use of such enzyme inhibitors as antiglaucoma drugs will be discussed in detail, together with the recent developments that led to isozyme-specific and organ-selective inhibitors.
Hypoxia activates the capacity of tumor‐associated carbonic anhydrase IX to acidify extracellular pH
It is shown that hypoxia regulates both expression and activity of CA IX in order to enhance the extracellular acidification, which may have important implications for tumor progression.
Characterization of CA XIII, a Novel Member of the Carbonic Anhydrase Isozyme Family*
The predicted amino acid sequence, structural model, distribution, and activity data suggest that CA XIII represents a novel enzyme, which may play important physiological roles in several organs.
Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition.
An unexpected nanomolar affinity is demonstrated of the COX-2 specific arylsulfonamide-type celecoxib and valdecoxib for isoenzymes of the totally unrelated carbonic anhydrase (CA) family, such as CA I, II, IV, and IX, whereas the rofecoxib methyl sulfone-type has no effect.
Crystal structure of the catalytic domain of the tumor-associated human carbonic anhydrase IX
On the basis of the structural differences observed between CA IX and the other membrane-associated α-CAs, further prospects for the rational drug design of isozyme-specific CA inhibitors are proposed, given that inhibition of this enzyme shows antitumor activity both in vitro and in vivo.
Biochemical Characterization of CA IX, One of the Most Active Carbonic Anhydrase Isozymes*
Investigations on the oligomerization and stability of the enzymes revealed that both recombinant proteins form dimers that are stabilized by intermolecular disulfide bond(s).
Targeting tumor hypoxia: suppression of breast tumor growth and metastasis by novel carbonic anhydrase IX inhibitors.
The findings show that CAIX is vital for growth and metastasis of hypoxic breast tumors and is a specific, targetable biomarker for breast cancer metastasis.
Crystal structure of a blue laccase from Lentinus tigrinus: evidences for intermediates in the molecular oxygen reductive splitting by multicopper oxidases
This is the first structure of a multicopper oxidase which allowed the detection of two intermediates in the molecular oxygen reduction and splitting, providing general insights into the reductive cleavage of the O-O bonds, a leading problem in many areas of biology.
Carbonic anhydrases as targets for medicinal chemistry.
Several important physiological and physio-pathological functions are played by CAs present in organisms all over the phylogenetic tree, related to respiration and transport of carbon dioxide to bicarbonate between metabolizing tissues and the lungs, pH and CO(2) homeostasis, electrolyte secretion in a variety of tissues/organs, biosynthetic reactions, such as the gluconeogenesis and ureagenesis among others.
Carbonic Anhydrase: Its Inhibitors and Activators
Carbonic Anhydrases: Catalytic and Inhibition Mechanisms, Distribution and Physiological RolesC.T. SupuranAcatalytic CAs: Carbonic Anhydrase-Related ProteinsI. NishimoriMultiple Binding Modes